| abstract |
The present invention relates to O-α-acyloxyalkyl ethers of venlafaxine metabolite 4- [2- (dimethylamino-1- (1-hydroxycyclohexyl) ethyl] phenol, or a pharmaceutically acceptable salt thereof Hydrates, R, S or RS forms thereof, and pharmaceutical compositions and methods for treating central nervous system diseases are provided.n n n Formula In n n n n n n n In Formula I,n n n The configuration at the stereogenic center (*) may be R, S or RS (racemate);n n n R 1 is selected from C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 3 -C 6 cycloalkyl and the residue of formula a;n n n Formula an n n n n n n n R 2 is selected from H and C 1 -C 6 alkyl; orn n n R 1 and R 2 are connected To form a moiety having the formula (b);n n n Formula bn n n n n n n n R 3 is selected from H and C 1 -C 6 alkyl;n n n R 4 and R 5 are H, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 thioalkoxy, -CN, -OH, -CF 3 , -OCF 3 , halogen, -NH 2 , -NO 2 , and mono or dialkylamino, wherein the alkyl groups each have 1 to 6 carbon atoms.n n n Venlafaxine, 4- [2- (dimethylamino-1- (1-hydroxycyclohexyl) ethyl] phenol, depression, schizophrenia, alcoholism, neuropathy. |